人肝细胞色素P450 2C金属酶与药物代谢  

Human Hepatic Cytochrome P450 2C Metalloenzymes and Drug Metabolism

作　　者：蒋华麟[1] 谭相石[1] 

机构地区：[1]复旦大学化学系生物医学研究院,上海200433

出　　处：《化学进展》2009年第5期911-918,共8页Progress in Chemistry

基　　金：国家自然科学基金项目(No.20771029);上海市重点学科基金项目(No.B108);上海市浦江计划项目(08PJ14017)资助

摘　　要：由于人肝细胞色素P4502C亚家族与临床药物代谢的密切关系,其研究已引起人们的广泛关注。本文综述了4种人肝细胞色素P4502C,着重综述了其中的三种:CYP2C9,CYP2C8,CYP2C19的研究进展。评述了CYP2C9,CYP2C8和CYP2C19的某些氨基酸残基在催化过程中的作用,这三种酶的基因多态在不同人种中的分布及药物代谢的差异,以及它们与用药的特异性及某些疾病的易感性的联系,介绍了目前提出的CYP2C8的底物药效团模型,最后总结了CYP2C9,CYP2C8,CYP2C19,CYP2C18的主要特性。Because of their close relationship to metabolism of clinically prescribed drugs, human hepatic cytochrome P450 2C subfamily has been paid wide attention. Research progress of four human hepatic cytochrome P450 2Cs are reviewed in this paper. Three of them, CYP2C9, CYP2C8, CYP2C19, are especially focused on. The functions of some of their amino acid residues, distribution in various ethnic groups and difference in metabolizing drugs of their polymorphisms, and their relationship with drug specificity and some diseases susceptibility are reviewed. A pharmacophore model of CYP2C8 substrate is introduced, and main characteristics of CYP2C9, CYP2C8, CYP2C19, CYP2C18 are summarized.

关 键 词：细胞色素P450 金属酶 基因多态性 用药特异性 

分 类 号：Q519[生物学—生物化学]